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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
Anionic cyclophanes as potential reversal agents of muscle relaxants by chemical chelation
Kenneth S Cameron1, Lee Fielding, Rona Mason
1Department of Analytical Chemistry, Organon Laboratories Ltd., Newhouse, Lanarkshire ML1 5SH, Scotland, UK.
Abstract:
A series of carboxyl-containing cyclophanes have been designed and synthesised as chemical chelators (or host molecules) of cationic muscle relaxant drugs (or guest molecules). Three of these cyclophane derivatives, 1-3, have been shown by NMR to form 1:1 complexes with the muscle relaxants pancuronium, and gallamine, in D(2)O, with association constants up to 10(4) M(-1). When tested in an in vitro chick biventer muscle preparation, the cyclophanes reversed the neuromuscular block induced by pancuronium and gallamine, with having the most effective reversal against pancuronium (EC(50) 40 microM.
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